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Purpose <p>Ebastine, a BCS Class II medication, serves as an antihistamine for treating various allergic reactions. However, its poor aqueous solubility and low oral bioavailability lead to extensive first-pass hepatic metabolism, significantly limiting its therapeutic effectiveness. To address these limitations, the current study aimed to develop and evaluate a nanofiber-based transdermal gel formulation to enhance Ebastine delivery through the skin.</p> Methods <p>Ebastine-loaded nanofibers were prepared using the electrospinning method and optimized with a “Box-Behnken experimental design.” The optimized formulation was incorporated into a gel for transdermal application. The formulation was evaluated using Scanning Electron Microscopy (SEM), Fourier-transform infrared spectroscopy (FTIR), in vitro drug release performed using a dialysis membrane, and ex vivo permeation tested through goat skin. Additionally, antimicrobial activity against <i>Staphylococcus aureus was</i> evaluated.</p> Result <p>The optimized NF5G2 formulation had a uniform diameter of less than 300&#xa0;nm with a higher drug entrapment efficiency of 95.23%. The cumulative drug release and skin permeation at 12&#xa0;h were 88.90% and 87.19%, respectively, following the Korsmeyer-Peppas kinetic model. The antimicrobial study showed significant inhibition of <i>S. aureus</i>, a common skin pathogen linked to chronic urticaria.</p> Conclusion <p>The developed Ebastine-loaded nanofiber transdermal gel offers improved drug release, high skin permeability, and effective antimicrobial action. This formulation presents a novel and efficient strategy for treating allergic conditions, paving the way for future applications of nanofiber-based therapies in dermatological care.</p> Graphical Abstract <p></p>

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Design, Development, and Optimization of Ebastine-Loaded Nanofibers-Dispersed Transdermal Gel for the Chronic Urticaria (Hives)

  • 期刊论文

  • 发表日期：

    2025年11月29日

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  • Bhushan Rane,
  • Puja Chaure,
  • Sanskruti Gawade,
  • Ashish Jain,
  • Abhay Shirode,
  • Yograj Kolhe

摘要

Purpose

Ebastine, a BCS Class II medication, serves as an antihistamine for treating various allergic reactions. However, its poor aqueous solubility and low oral bioavailability lead to extensive first-pass hepatic metabolism, significantly limiting its therapeutic effectiveness. To address these limitations, the current study aimed to develop and evaluate a nanofiber-based transdermal gel formulation to enhance Ebastine delivery through the skin.

Methods

Ebastine-loaded nanofibers were prepared using the electrospinning method and optimized with a “Box-Behnken experimental design.” The optimized formulation was incorporated into a gel for transdermal application. The formulation was evaluated using Scanning Electron Microscopy (SEM), Fourier-transform infrared spectroscopy (FTIR), in vitro drug release performed using a dialysis membrane, and ex vivo permeation tested through goat skin. Additionally, antimicrobial activity against Staphylococcus aureus was evaluated.

Result

The optimized NF5G2 formulation had a uniform diameter of less than 300 nm with a higher drug entrapment efficiency of 95.23%. The cumulative drug release and skin permeation at 12 h were 88.90% and 87.19%, respectively, following the Korsmeyer-Peppas kinetic model. The antimicrobial study showed significant inhibition of S. aureus, a common skin pathogen linked to chronic urticaria.

Conclusion

The developed Ebastine-loaded nanofiber transdermal gel offers improved drug release, high skin permeability, and effective antimicrobial action. This formulation presents a novel and efficient strategy for treating allergic conditions, paving the way for future applications of nanofiber-based therapies in dermatological care.

Graphical Abstract